Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, Hamdard Nagar, New Delhi, 110062, India.
AAPS PharmSciTech. 2019 Jan 8;20(2):60. doi: 10.1208/s12249-018-1284-9.
The therapeutic functionality of innumerable antiretroviral drugs is supposedly obscured owing to their low metabolic stability in the gastrointestinal tract and poor solubilization property leading to poor oral bioavailability. Dictated by such needs, lipid-based formulations could be tailored using nanotechnology which would be instrumental in ameliorating the attributes of such drugs. The stupendous advantages which lipid nanocarriers offer including improved drug stability and peroral bioavailability coupled with sustained drug release profile and feasibility to incorporate wide array of drugs makes it a potential candidate for pharmaceutical formulations. Furthermore, they also impart targeted drug delivery thereby widening their arena for use. Therefore, the review will encompass the details pertaining to numerous lipid nanocarriers such as nanoemulsion, solid lipid nanoparticle, nanostructured lipid carriers, and so on. These nanocarriers bear the prospective of improving the mucosal adhesion property of the drugs which ultimately upgrades its pharmacokinetic profile. The biodegradable and physiological nature of the lipid excipients used in the formulation is the key parameter and advocates for their safe use. Nevertheless, these lipid-based nanocarriers are amenable to alterations which could be rightly achieved by changing the excipients used or by modifying the process parameters. Thus, the review will systematically envisage the impending benefits and future perspectives of different lipid nanocarriers used in oral delivery of antiretroviral drugs.
由于在胃肠道中代谢稳定性低和溶解性能差导致口服生物利用度低,无数抗逆转录病毒药物的治疗功能据称被掩盖了。出于这种需求,使用纳米技术可以定制基于脂质的制剂,这将有助于改善这些药物的特性。脂质纳米载体具有许多巨大的优势,包括提高药物稳定性和口服生物利用度,加上药物持续释放的特点,以及能够纳入广泛的药物,这使其成为药物制剂的潜在候选者。此外,它们还赋予靶向药物递送,从而扩大了其使用范围。因此,本综述将涵盖有关各种脂质纳米载体的详细信息,例如纳米乳液、固体脂质纳米粒、纳米结构脂质载体等。这些纳米载体有望提高药物的粘膜黏附特性,从而改善其药代动力学特性。在制剂中使用的脂质赋形剂的可生物降解和生理性质是关键参数,这为其安全使用提供了依据。然而,这些基于脂质的纳米载体容易发生变化,可以通过改变使用的赋形剂或修改工艺参数来实现。因此,本综述将系统地预见不同脂质纳米载体在抗逆转录病毒药物口服递送上的预期益处和未来前景。